基于碎片的药物发现活动,以原生质谱法为指导
Louise M Sternicki1,2, Sally-Ann Poulsen1,2
1Griffith Institute for Drug Discovery, Griffith University Nathan Brisbane Queensland 4111 Australia s.poulsen@griffith.edu.au.
RSC medicinal chemistry
|July 19, 2024
概括
原生质谱 (nMS) 通过灵敏地检测弱联体相互作用来推进基于碎片的药物发现 (FBDD). 本审查更新了2014-2023年nMS对FBDD的贡献,突出了其超出可溶性蛋白质的扩大作用.
科学领域:
- 生物物理技术 生物物理技术
- 药物发现 药物发现
- 分析化学是一种分析化学.
背景情况:
- 原生质谱法 (nMS) 是一种敏感的生物物理方法,用于表征生物分子及其相互作用.
- 它的高灵敏度对于检测基于片段的药物发现 (FBDD) 中的弱结合联体至关重要.
研究的目的:
- 提供自2014年至2023年为基于碎片的药物发现提供原生质谱学的贡献的最新审查.
- 将nMS在FBDD中的发展与其他生物物理查技术相结合.
- 讨论nMS在药物发现中的未来潜力和扩展应用.
主要方法:
- 在FBDD (2014-2023) 中对原生质谱应用的文献综述.
- 对nMS与其他生物物理碎片选方法进行比较分析.
- 在治疗领域探索新兴的nMS应用.
主要成果:
- 在过去的十年中,原生质谱显著指导了FBDD击中识别和表征.
- 在FBDD中,nMS的采用量有所增长,证明了它的实用性和敏感性.
- 这种技术显示出对超出可溶性蛋白质的查有前途,包括PROTACs,RNA结合分子和共价疗法.
结论:
- 原生质谱是一种强大且越来越多地被采用的基于片段的药物发现技术.
- 它的应用范围正在扩大,为治疗开发提供了新的途径.
- 在nMS的持续进步将进一步增强其在识别新药候选者的作用.
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